A facile large scale synthesis of optically active 3-amino-5-(2-pyridyl)-1,4-benzodiazepin-2-one derivatives |
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| Authors: | Graeme Semple Hamish Ryder Mitsuaki Ohta Masato Satoh |
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| Affiliation: | 1. Ferring Research Institute, Chilworth Research Centre , Chilworth, Southampton, U.K. , S016 7NP;2. Neuroscience &3. Gastrointestinal Research Laboratories , Yamanouchi Institute for Drug Discovery Research , 21, Miyukigaoka, Tsukuba, Ibaraki, 305, Japan |
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| Abstract: | ![]()
A facile method for the synthesis of 3-amino-5-(2-pyridyl)-1,4-benzodiazepin-2-ones (8) mediated by benzotriazole is described. The synthesis and optical resolution of the product by fractional crystallisation proceeds in high yield, under mild conditions and without recourse to toxic reagents or chromatographic separations and hence is amenable to the large scale preparation of these important precursors to potent CCK receptor ligands. |
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| Keywords: | Mo(CO)6 Azides Nitro compounds Selective reduction Neutral |
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